102437-03-6Relevant articles and documents
SUBSTITUTED 5-CYANOINDOLE COMPOUNDS AND USES THEREOF
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Paragraph 00274; 00287, (2019/01/10)
A compound of Formula (I), or a pharmaceutically acceptable salt thereof, is provided that has been shown to be useful for the treatment of lysine (K)-specific demethylase 1A (LSD1) - mediated diseases or disorders, Formula (I), wherein R1, R2, R3, R4, and R5 are as defined herein.
A pharmaceutical intermediate 4 - (4 - chlorophenyl) cyclohexyl -1 - formic acid
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Paragraph 0032; 0033; 0041, (2017/04/19)
The invention belongs to the field of preparation of drug intermediates and particularly relates to a synthesis method of a drug intermediate 4-(4-chlorphenyl) cyclohexyl-1-formic acid. The method comprises the following steps: firstly reacting a compound I with R2SO2Cl in the presence of an acid-binding agent to obtain a compound II; carrying out catalytic coupling reaction on the compound II and a Grignard reagent 4-chlorphenyl magnesium halide under the action of a catalyst to obtain a compound III; and finally hydrolyzing the compound III in alkali liquor to obtain a target product 4-(4-chlorphenyl) cyclohexyl-1-formic acid. According to the synthesis method, all steps in a reaction route are exclusive reactions; and ortho-position and meta-position problems in friedel-crafts reaction are overcome, so that the utilization rate of raw materials is high; the total yield is high; and the cost is low. A main body structure is constructed by a coupling technique, so that the problem that hydrolysate which is formed after a lot of lewis acid used in the friedel-crafts reaction is hydrolyzed needs to be subjected to special treatment is overcome; the method is environment-friendly; and industrialized production is facilitated.
BIARYL COMPOUNDS USEFUL FOR THE TREATMENT OF HUMAN DISEASES IN ONCOLOGY, NEUROLOGY AND IMMUNOLOGY
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Paragraph 0241, (2015/06/25)
The present invention provides compounds and compositions thereof which are useful as inhibitors of Bruton's tyrosine kinase and which exhibit desirable characteristics for the same.
General Syntheses of 6- and 7-Carbomethoxy-trans-1-heteradecalins and 6- and 7-Carbomethoxy-trans-2-heteradecalins
Hirsch, Jerry A.,Truc, Vu Chi
, p. 2218 - 2227 (2007/10/02)
Two routes to all of the title compounds in the oxa and aza series have been studied.The most general path, involving a cyclohexene oxide intermediate, was not successful becauase of difficulty in separating regioisomers.Allylation of 4-carbomethoxycyclohexanone (11) followed by reduction produced the required trans-disubstituted allyl alcohols, which were converted to all of the desired 6-carbomethoxy-trans-1-heteradecalins.The allyl ketones were subjected to a homologation-side chain contraction sequence to produce the 6-carbomethoxy-trans-2-heteradecalins.Allylation of 3-carbomethoxycyclohexanone (12) was not regioselective, but all four product isomers were characterized.The desired 5-carbomethoxy-2-allylcyclohexanone isomers (27 and 28) were converted to the 7-carbomethoxy-trans-decalins by similar series of reactions